- Triple-Bond Directed Csp2?N Bond Formation with N-Fluorobenzenesulfonimide as Aminating Source: One-Step Transformation of Aldehydes into Amines
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A metal-free, versatile triple-bond directed approach for the decarbonylative C?H amination of ortho-alkynyl quinoline/pyridine aldehydes using N-fluorobenzenesulfonimide as nitrogen source under mild reaction conditions has been described. The designed reaction strategy was triggered by trapping of fluorine by base with subsequent attack of bis(phenylsulfonyl)-λ2-azane on the carbonyl carbon of a heterocycle, which was gradually converted into the corresponding amine through a Curtius type rearrangement. This protocol provides a one-step approach for the conversion of aldehydes into amines in good yields. The synthesized amines were successfully transformed into biologically important pyrroloquinolines/pyridines.
- Sushmita,Aggarwal, Trapti,Shibata, Norio,Verma, Akhilesh K.
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- Facile synthesis of 2-substituted 4-azaindoles
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A novel and efficient strategy for the synthesis of 2-substituted 4-azaindoles from 2-chloro-3-nitropyridine through Pd-catalyzed Sonogashira cross-coupling, followed by reduction and heteroannulation on t-BuOK, is reported. Copyright Taylor & Francis Group, LLC.
- Sun, Li-Ping,Wang, Jin-Xin
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p. 2187 - 2193
(2008/02/05)
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- AMIDE DERIVATIVES AND DRUGS
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The present invention provides an amide derivative represented by the following formula [1]: wherein n represents 0 or 1; X represents CR4 or N; Y represents CR6 or N; Z represents CR7 or N; R1 and R2 may be the same or different and each represents hydrogen, optionally substituted alkyl, acyl, optionally substituted aryl, or an optionally substituted aromatic heterocyclic group; R4, R5, R6 and R7 may be the same or different and each represents hydrogen, halogen, hydroxy, amino, alkyl, haloalkyl, alkoxy, monoalkylamino, dialkylamino, arylalkyl, cyano, or nitro; and R3 represents optionally substituted alkylamino, optionally substituted arylamino, or optionally substituted cyclic amino, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising them as an active ingredient. The compound of the present invention is useful as a TGF-β inhibitor.
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- Synthesis of polyfunctional indoles and related heterocycles mediated by cesium and potassium bases
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A general preparation of 2-substituted indoles starting from functionalized 2-alkynylanilines has been developed. This base mediated reaction has also been used to synthesize the heterocyclic core of the marine alkaloid hinckdentine A. Furthermore the reaction was successfully adapted to the solid phase. Benzofurans and isoindolones could also be prepared with this method.
- Koradin, Christopher,Dohle, Wolfgang,Rodriguez, Alain L.,Schmid, Bertram,Knochel, Paul
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p. 1571 - 1587
(2007/10/03)
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